engleski

Development and in vitro assessment of phospholipid nanovesicles for vaginal delivery of azithromycin

The goal of this study was to develop and evaluate the abilities of azithromycin (AZI)- loaded liposomes for topical vaginal treatment of recurrent bacterial infections. Size and surface properties of different AZI liposomes, i.e. propylene glycol liposomes (PGLs), deformable propylene glycol liposomes (DPGLs) and conventional liposomes (CLs), were evaluated by photon correlation spectroscopy [1] at neutral and acidic conditions (pH 4.5). Ex vivo vaginal deposition/penetration studies were performed by Franz cell diffusion method using porcine vaginal tissue [2]. The anti- biofilm potential of the different AZI- liposomes was assessed in two modes, pre- and post-biofilm formation [3], and the obtained activities were compared with those achieved with AZI-solution. All AZI-liposomes increased in their mean diameters and polydispersity indexes, while decreased in zeta potential values at simulated vaginal conditions (pH 4.5), as compared to the values obtained at pH 7.5. The performed ex vivo studies proved the potentials of AZI- liposomes in topical vaginal therapy, where all the tested liposomes enabled accumulation of the antibiotic on vaginal surface and inside vaginal tissue, reducing undesired penetration to systemic circulation. CLs were the most effective at preventing formation of E. coli 700928 and K-12 biofilms with IC50 values (concentrations inhibiting biofilm viability by 50 %) up to 8-fold lower than those of AZI- solution, while DPGLs exhibited the highest potential in eradication of already formed E. coli biofilms. The presented studies confirm the potentials of using AZI-liposomes for topical vaginal therapy of recurrent bacterial infections.

Phospholipids ; Deformable liposomes ; Propylene glycol liposomes ; Azithromycin

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